Catalog Number: 2228
Alternate Names: HWA 486, RS-34821
Chemical Name: 5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
Biological Activity
Inhibitor of dihydroorotate dehydrogenase (IC50 = 2.5 μM). Inhibits de novo pyrimidine synthesis in human T cells in vitro; also inhibits lymphocyte proliferation. Exhibits efficacy in several animal models of autoimmune disease, arthritis and graft rejection. Active metabolite, teriflunomide (A77 1726, Cat. No. 5069), also available.
Technical Data
  • M.Wt:
    270.21
  • Formula:
    C12H9F3N2O2
  • Solubility:
    Soluble to 100 mM in ethanol and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    75706-12-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The immunosuppressant leflunomide inhibits lymphocyte proliferation by inhibiting pyrimidine biosynthesis.
    Cherwinski et al.
    J.Pharmacol.Exp.Ther., 1995;275:1043
  2. Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide.
    Brazelton and Morris
    Curr.Opin.Immunol., 1996;8:710
  3. Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide.
    Greene et al.
    Biochem.Pharmacol., 1995;50:861
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Leflunomide include:

1 Citations: Showing 1 - 1

  1. Interleukin-13 inhibits proliferation and enhances contractility of human airway smooth muscle cells without change in contractile phenotype.
    Authors: Risse Et al.
    J Biomol Res Ther 2011;300:L958

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